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Purity: ≥98%
HA130 (HA-130) is a novel, potent and selective inhibitor of autotaxin (ATX, IC50 = 28 nM) with anticancer activity. HA130 inhibits the enzymatic activity of ATX, and slows T cell migration across lymph node HEVs in vivo. Ex vivo, HA130 blunts the TEM-promoting activity of ATX, paralleling its in vivo effects. Autotaxin (ATX) is an ectoenzyme that catalyzes the conversion of lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), a bioactive lipid and a close relative of sphingosine 1-phosphate.
| ln Vitro |
The capacity of ATX to stimulate TEM (transendothelial migration) is totally inhibited by HA130. At 0.3 μM, HA130 totally eliminated ATX's activity on TK1 tail-foot formation [1].
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| ln Vivo |
HEV migration of T cells across lymph nodes is slowed by HA130. Comparing animals treated with HA130 to those not, the "external HEV/internal HEV" ratio is lowered by 3–4 times [1]. When HA130 is injected subcutaneously, draining lymph nodes (LN) experience a notable increase in lymphocytes within the endothelial cell (EC) and sub-EC layers of HEV [2].
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| References |
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| Molecular Formula |
C24H19BFNO5S
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|---|---|
| Molecular Weight |
463.2858
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| Exact Mass |
463.106
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| CAS # |
1229652-21-4
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| PubChem CID |
46911532
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.258
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
722
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| Defined Atom Stereocenter Count |
0
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| SMILES |
B(C1=CC(=CC=C1)COC2=CC=C(C=C2)/C=C\3/C(=O)N(C(=O)S3)CC4=CC=C(C=C4)F)(O)O
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| InChi Key |
VTNKMYWFWQTEHE-XKZIYDEJSA-N
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| InChi Code |
InChI=1S/C24H19BFNO5S/c26-20-8-4-17(5-9-20)14-27-23(28)22(33-24(27)29)13-16-6-10-21(11-7-16)32-15-18-2-1-3-19(12-18)25(30)31/h1-13,30-31H,14-15H2/b22-13-
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| Chemical Name |
(Z)-(3-((4-((3-(4-fluorobenzyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)methyl)phenyl)boronic acid
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| Synonyms |
HA-130; HA130; HA 130
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 39 mg/mL (~84.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1585 mL | 10.7924 mL | 21.5848 mL | |
| 5 mM | 0.4317 mL | 2.1585 mL | 4.3170 mL | |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1585 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 HA130 impedes T cell entry into lymph nodes.J Immunol.2012 Oct 15;189(8):3914-24. |
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 Binding of ATX to T cells.J Immunol.2012 Oct 15;189(8):3914-24. |
 ATX induces motility of na.J Immunol.2012 Oct 15;189(8):3914-24. |
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